An antibiotic with antitumor properties. A cell-permeable potent and selective inhibitor of farnesyltransferase (FTase; IC50 = 5 µM) compared to geranylgeranyltransferase I (GGTase I; IC50 = 180 µM). Manumycin acts as a competitive inhibitor of FTase with respect to farnesylpyrophosphate (FPP; Ki = 1.2 µM), but acts as a noncompetitive inhibitor with respect to the Ras acceptor protein. Reported to inhibit the growth and invasive activity of pancreatic cancer cells.
Biochem/physiol Actions
Primary Target Farnesyltransferase (FTAse)
Target IC50: 5 µM against farnesyltransferase (FTase); 180 µM against geranylgeranyltransferase I (GGTase I)
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C).
Other Notes
Kainuma, O., et al. 1997. Pancreas15, 379. Nagase, T., et al. 1996. Int. J. Cancer 65, 620. Hara, M., et al. 1995. Proc. Natl. Acad. Sci. USA92, 3333. Hara, M., et al. 1993. Proc. Natl. Acad. Sci. USA90, 2281. Tamanoi, R. 1993. Trends Biochem. Sci.18, 349.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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